Pacritinib-d₄  (Synonyms: SB1518-d₄)

Pacritinib-d₈ (SB1518-d₈) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits FLT3 (IC₅₀=22 nM) and its mutant FLT3^D835Y (IC₅₀=6 nM).

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB1518-d4

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

476.60

C₂₈H₂₈D₄N₄O₃

937272-79-2

[2H]C(CCC1([2H])[2H])([2H])N1CCOC(C=C2)=C3COC/C=C/COCC4=CC=CC(C5=N/C(NC=C5)=N\C2=C3)=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. William AD, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JA  [Content Brief]

  [2]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011 Nov;1(11):e44.  [Content Brief]

  [3]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9.  [Content Brief]